Refereed journal article or data article (A1)

Synthesis of an Alkyne-Modified Bleomycin Disaccharide Precursor, Conversion to a F-18-Labeled Radiotracer, and Preliminary in vivo-PET Imaging Studies




List of AuthorsSajal K. Maity, Cheng-Bin Yim, Satish Jadhav, Alejandra Verhassel, Johanna Tuomela, Olof Solin, Tove J. Grönroos, Pasi Virta

PublisherWILEY-V C H VERLAG GMBH

Publication year2019

JournalEuropean Journal of Organic Chemistry

Journal name in sourceEUROPEAN JOURNAL OF ORGANIC CHEMISTRY

Journal acronymEUR J ORG CHEM

Volume number2019

Issue number1

Start page156

End page163

Number of pages8

ISSN1434-193X

eISSN1099-0690

DOIhttp://dx.doi.org/10.1002/ejoc.201801488

Self-archived copy’s web addresshttps://research.utu.fi/converis/portal/detail/Publication/39298097


Abstract
The bleomycins (BLMs) are known antitumor antibiotics composed of the tumoricidal and tumor seeking domains. The peptide structure of BLMs is responsible for the cytotoxicity by selective oxidative cleavage of DNA (and RNA), while the tumor cell selectivity and internalization resides in the disaccharide moiety (i.e. BLM disaccharide). This has prompted researchers to utilize BLM disaccharide and its derivatives as constituents for the selective recognition of tumor cells, which may find further applications as new tumor imaging tools or drug delivery vehicles. In the present study a high yielding synthesis of an alkyne modified BLM disaccharide precursor that may be used as a useful agent for the click conjugation, its conversion to a F-18-labeled radiotracer, and preliminary in vivo PET imaging studies of the tracer with breast cancer (MCF-7) xenograft mouse models are described.

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Last updated on 2022-07-04 at 17:15